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Vol. 295, Issue 1, 139-145, October 2000
Novartis Pharma AG, Oncology Research, CH-4002 Basel, Switzerland
(E.B., N.L., N.B.L.); Novartis Pharma, Summit, New Jersey (C.L.C.); and
Division of Hematology and Medical Oncology, Oregon Health Sciences
University, Portland, Oregon (S.O.-J., B.J.D.)
STI571 (formerly known as CGP 57148B) is a protein-tyrosine kinase
inhibitor that is currently in clinical trials for the treatment of
chronic myelogenous leukemia. STI571 selectively inhibits the
Abl and platelet-derived growth factor (PDGF) receptor tyrosine kinases
in vitro and blocks cellular proliferation and tumor growth of
Bcr-abl- or v-abl-expressing cells. We
have further investigated the profile of STI571 against related
receptor tyrosine kinases. STI571 was found to potently inhibit the
kinase activity of the 
- and 
-PDGF receptors and the receptor for
stem cell factor, but not the closely related c-Fms, Flt-3, Kdr, Flt-1, and Tek tyrosine kinases. Additionally, no inhibition of c-Met or nonreceptor tyrosine kinases such as Src and Jak-2 has been observed. In cell-based assays, STI571 selectively inhibited PDGF and
stem cell factor-mediated cellular signaling, including
ligand-stimulated receptor autophosphorylation, inositol phosphate
formation, and mitogen-activated protein kinase activation and
proliferation. These results expand the profile of STI571 and suggest
that in addition to chronic myelogenous leukemia, STI571 may have
clinical potential in the treatment of diseases that involve abnormal
activation of c-Kit or PDGF receptor tyrosine kinases.
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M. M. Schittenhelm, S. Shiraga, A. Schroeder, A. S. Corbin, D. Griffith, F. Y. Lee, C. Bokemeyer, M. W.N. Deininger, B. J. Druker, and M. C. Heinrich Dasatinib (BMS-354825), a Dual SRC/ABL Kinase Inhibitor, Inhibits the Kinase Activity of Wild-Type, Juxtamembrane, and Activation Loop Mutant KIT Isoforms Associated with Human Malignancies Cancer Res., January 1, 2006; 66(1): 473 - 481. [Abstract] [Full Text] [PDF]
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R. S. Benjamin, C. D. Blanke, J.-Y. Blay, S. Bonvalot, and B. Eisenberg Management of Gastrointestinal Stromal Tumors in the Imatinib Era: Selected Case Studies Oncologist, January 1, 2006; 11(1): 9 - 20. [Abstract] [Full Text] [PDF]
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G. Rossi, A. Cavazza, A. Marchioni, L. Longo, M. Migaldi, G. Sartori, N. Bigiani, L. Schirosi, C. Casali, U. Morandi, et al. Role of Chemotherapy and the Receptor Tyrosine Kinases KIT, PDGFR{alpha}, PDGFR{beta}, and Met in Large-Cell Neuroendocrine Carcinoma of the Lung J. Clin. Oncol., December 1, 2005; 23(34): 8774 - 8785. [Abstract] [Full Text] [PDF]
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K. Yokoi, T. Sasaki, C. D. Bucana, D. Fan, C. H. Baker, Y. Kitadai, T. Kuwai, J. L. Abbruzzese, and I. J. Fidler Simultaneous Inhibition of EGFR, VEGFR, and Platelet-Derived Growth Factor Receptor Signaling Combined with Gemcitabine Produces Therapy of Human Pancreatic Carcinoma and Prolongs Survival in an Orthotopic Nude Mouse Model Cancer Res., November 15, 2005; 65(22): 10371 - 10380. [Abstract] [Full Text] [PDF]
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C. Cutcliffe, D. Kersey, C.-C. Huang, Y. Zeng, D. Walterhouse, E. J. Perlman, and for the Renal Tumor Committee of the Children's On Clear Cell Sarcoma of the Kidney: Up-regulation of Neural Markers with Activation of the Sonic Hedgehog and Akt Pathways Clin. Cancer Res., November 15, 2005; 11(22): 7986 - 7994. [Abstract] [Full Text] [PDF]
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R. Tussiwand, N. Onai, L. Mazzucchelli, and M. G. Manz Inhibition of Natural Type I IFN-Producing and Dendritic Cell Development by a Small Molecule Receptor Tyrosine Kinase Inhibitor with Flt3 Affinity J. Immunol., September 15, 2005; 175(6): 3674 - 3680. [Abstract] [Full Text] [PDF]
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T. A. Carter, L. M. Wodicka, N. P. Shah, A. M. Velasco, M. A. Fabian, D. K. Treiber, Z. V. Milanov, C. E. Atteridge, W. H. Biggs III, P. T. Edeen, et al. Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases PNAS, August 2, 2005; 102(31): 11011 - 11016. [Abstract] [Full Text] [PDF]
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A. S. Corbin, S. Demehri, I. J. Griswold, Y. Wang, C. A. Metcalf III, R. Sundaramoorthi, W. C. Shakespeare, J. Snodgrass, S. Wardwell, D. Dalgarno, et al. In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit Blood, July 1, 2005; 106(1): 227 - 234. [Abstract] [Full Text] [PDF]
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C. Tarn, E. Merkel, A. A. Canutescu, W. Shen, Y. Skorobogatko, M. J. Heslin, B. Eisenberg, R. Birbe, A. Patchefsky, R. Dunbrack, et al. Analysis of KIT Mutations in Sporadic and Familial Gastrointestinal Stromal Tumors: Therapeutic Implications through Protein Modeling Clin. Cancer Res., May 15, 2005; 11(10): 3668 - 3677. [Abstract] [Full Text] [PDF]
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C. Renne, K. Willenbrock, R. Kuppers, M.-L. Hansmann, and A. Brauninger Autocrine- and paracrine-activated receptor tyrosine kinases in classic Hodgkin lymphoma Blood, May 15, 2005; 105(10): 4051 - 4059. [Abstract] [Full Text] [PDF]
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X.-F. Zhu, B.-F. Xie, J.-M. Zhou, G.-K. Feng, Z.-C. Liu, X.-Y. Wei, F.-X. Zhang, M.-F. Liu, and Y.-X. Zeng Blockade of Vascular Endothelial Growth Factor Receptor Signal Pathway and Antitumor Activity of ON-III (2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone), a Component from Chinese Herbal Medicine Mol. Pharmacol., May 1, 2005; 67(5): 1444 - 1450. [Abstract] [Full Text] [PDF]
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A. L. Dewar, A. C. Cambareri, A. C. W. Zannettino, B. L. Miller, K. V. Doherty, T. P. Hughes, and A. B. Lyons Macrophage colony-stimulating factor receptor c-fms is a novel target of imatinib Blood, April 15, 2005; 105(8): 3127 - 3132. [Abstract] [Full Text] [PDF]
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M. Deininger, E. Buchdunger, and B. J. Druker The development of imatinib as a therapeutic agent for chronic myeloid leukemia Blood, April 1, 2005; 105(7): 2640 - 2653. [Abstract] [Full Text] [PDF]
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S. Appel, A. Rupf, M. M. Weck, O. Schoor, T. H. Brummendorf, T. Weinschenk, F. Grunebach, and P. Brossart Effects of Imatinib on Monocyte-Derived Dendritic Cells Are Mediated by Inhibition of Nuclear Factor-{kappa}B and Akt Signaling Pathways Clin. Cancer Res., March 1, 2005; 11(5): 1928 - 1940. [Abstract] [Full Text] [PDF]
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K. Pietras and D. Hanahan A Multitargeted, Metronomic, and Maximum-Tolerated Dose "Chemo-Switch" Regimen is Antiangiogenic, Producing Objective Responses and Survival Benefit in a Mouse Model of Cancer J. Clin. Oncol., February 10, 2005; 23(5): 939 - 952. [Abstract] [Full Text] [PDF]
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Y.-Y. Wang, G.-B. Zhou, T. Yin, B. Chen, J.-Y. Shi, W.-X. Liang, X.-L. Jin, J.-H. You, G. Yang, Z.-X. Shen, et al. AML1-ETO and C-KIT mutation/overexpression in t(8;21) leukemia: Implication in stepwise leukemogenesis and response to Gleevec PNAS, January 25, 2005; 102(4): 1104 - 1109. [Abstract] [Full Text] [PDF]
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S. Wang, M. C. Wilkes, E. B. Leof, and R. Hirschberg Imatinib mesylate blocks a non-Smad TGF-{beta} pathway and reduces renal fibrogenesis in vivo FASEB J, January 1, 2005; 19(1): 1 - 11. [Abstract] [Full Text] [PDF]
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H. Sihto, M. Sarlomo-Rikala, O. Tynninen, M. Tanner, L. C. Andersson, K. Franssila, N. N. Nupponen, and H. Joensuu KIT and Platelet-Derived Growth Factor Receptor Alpha Tyrosine Kinase Gene Mutations and KIT Amplifications in Human Solid Tumors J. Clin. Oncol., January 1, 2005; 23(1): 49 - 57. [Abstract] [Full Text] [PDF]
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K. W. H. Yee, M. Schittenhelm, A.-M. O'Farrell, A. R. Town, L. McGreevey, T. Bainbridge, J. M. Cherrington, and M. C. Heinrich Synergistic effect of SU11248 with cytarabine or daunorubicin on FLT3 ITD-positive leukemic cells Blood, December 15, 2004; 104(13): 4202 - 4209. [Abstract] [Full Text] [PDF]
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A. S. Corbin, I. J. Griswold, P. La Rosee, K. W. H. Yee, M. C. Heinrich, C. L. Reimer, B. J. Druker, and M. W. N. Deininger Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970 Blood, December 1, 2004; 104(12): 3754 - 3757. [Abstract] [Full Text] [PDF]
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H. Burger, H. van Tol, A. W. M. Boersma, M. Brok, E. A. C. Wiemer, G. Stoter, and K. Nooter Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ABCG2 drug pump Blood, November 1, 2004; 104(9): 2940 - 2942. [Abstract] [Full Text] [PDF]
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A. Pardanani and A. Tefferi Imatinib targets other than bcr/abl and their clinical relevance in myeloid disorders Blood, October 1, 2004; 104(7): 1931 - 1939. [Abstract] [Full Text] [PDF]
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